Browsing by Author "Demiroglu, H"

Now showing 1 - 11 of 11
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    Radiosynthesis and biodistribution of 99mTc-Sulfamethoxazole: a novel molecule for in-vivo infection imaging
    Uyaroglu, Ö; Demiroglu, H; Topal, G; Parlak, Y; Gümüser, FG; Türköz, EU; Demir, V; Ates, B; Ünak, P; Avcibasi, U
    The aim of this study was to prepare Tc-99m-Sulfamethoxazole complex and evaluate its efficiency as an infection imaging agent. The Sulfamethoxazole was labeled with Tc-99m and its biological efficacy as a potential radio tracer for Staphylococcus aureus infection was investigated in bacterially infected Albino Wistar rats. The radiolabeling yield was found to be 95 +/- 3.07% and remained constant at more than 93 +/- 0.1% even in serum for 240 min after radiolabeling. Tc-99m-Sulfamethoxazole prepared with high yield localized well in the bacterially infected muscle of the rats. Tc-99m-Sulfamethoxazole may be developed as a radiopharmaceutical agent to distinguish infection from inflammation by nuclear imaging.
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    Metabolic Comparison of Radiolabeled Bleomycin and Bleomycin-Glucuronide Labeled with 99mTc
    Koçan, F; Avcibasi, U; Ünak, P; Müftüler, FZB; Içhedef, ÇA; Demiroglu, H; Gümüser, FG
    The metabolic comparison of bleomycin (BLM) and bleomycin-glucuronide (BLMG) radiolabeled with Tc-99m (Tc-99m-BLM and Tc-99m-BLMG, respectively) has been investigated in this study. Quality control procedures were carried out using thin-layer radiochromatography and high-performance liquid chromatography. To compare the metabolic behavior of BLM and its glucuronide conjugate radiolabeled with Tc-99m, scintigraphic, and biodistributional techniques were applied using male New Zealand rabbits and Albino Wistar rats. The results obtained have shown that these compounds were successfully radiolabeled with a labeling yield of about 100%. Maximum uptakes of Tc-99m-BLM and Tc-99m-BLMG metabolized as N-glucuronide were observed within 2 hours in the liver, the bladder, and the spinal cord for Tc-99m-BLM and the lung, the liver, the kidney, the large intestine, and the spinal cord for Tc-99m-BLMG, respectively. Scintigraphy and biodistributional studies performed on the experimental animals have shown that radiopharmaceutical potentials of these compounds are completely different. At the same time, uptake of the Tc-99m-BLMG was found to be better than that of Tc-99m-BLM.
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    Radiosynthesis and Biodistribution of 99mTc-Trimethoprim: A Novel Radiolabeled Antibiotic for Bacterial Infection Imaging Using Experimental Animals
    Demiroglu, H; Topal, G; Parlak, Y; Gümüser, FG; Türköz, EU; Tekin, V; Ates, B; Ünak, P; Avcibasi, U
    In the present article, we focused on the radiolabeling and evaluation of Tc-99m-TMH complex as a potential candidate for infection imaging in vivo. For this; Trimethoprim (TMH) used to treat bacterial infections was investigated to label with Tc-99m. Labeling was performed using thin (II) chloride as a reducing agent at room temperature for 1 h and radiochemical analysis involved thin layer radiochromatography (TLRC) and high pressure liquid radiochromatograpy (HPLRC) methods. The stability of labeled antibiotic was checked in the presence of rat blood serum at 37 degrees C up to 180 min. The maximum radiolabeling yield was found to be 96 +/- 2% and remained constant at more than 85 +/- 1% even in rat serum for 180 min after radiolabeling. Static image of Tc-99m-TMH in male rats demonstrated that important radiation signals are present in the infected site at first glance in 30 min. After 30 min the uptake of the Tc-99m-TMH as ID/g% in the infected muscle (INM) and normal muscle (NM) of the rats were 7.5 +/- 1.5% and 5.00 +/- 1.2%, respectively. In the INM/NM ratio a desirable behavior was observed as the values for the INM/NM increased up to 10.6. Tc-99m-TMH prepared with high yield is able to localize well in the bacterially infected muscle of the rats. As a result, Tc-99m-TMH may be developed as a radiopharmaceutical agent to distinguish infection from inflammation by nuclear imaging.
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    Radiolabeling of new generation magnetic poly(HEMA-MAPA) nanoparticles with 131I and preliminary investigation of its radiopharmaceutical potential using albino Wistar rats
    Avcibasi, U; Demiroglu, H; Ediz, M; Akalin, HA; Özçaliskan, E; Senay, H; Türkcan, C; Özcan, Y; Akgöl, S; Avcibasi, N
    In this study, N-methacryloyl-l-phenylalanine (MAPA) containing poly(2-hydroxyethylmethacrylate) (HEMA)-based magnetic poly(HEMA-MAPA) nanobeads [mag-poly(HEMA-MAPA)] were radiolabeled with I-131 [I-131-mag-poly(HEMA-MAPA)], and the radiopharmaceutical potential of I-131-mag-poly(HEMA-MAPA) was investigated. Quality control studies were carried out by radiochromatographic method to be sure that I-131 binded to mag-poly(HEMA-MAPA) efficiently. In this sense, binding yield of I-131-mag-poly(HEMA-MAPA) was found to be about 95-100%. In addition to this, optimum radiodination conditions for I-131-mag-poly(HEMA-MAPA) were determined by thin-layer radiochromatography studies. In addition to thin-layer radiochromatography studies, lipophilicity (partition coefficient) and stability studies for I-131-mag-poly(HEMA-MAPA) were realized. It was determined that lipophilicities of mag-poly(HEMA-MAPA) and I-131-mag-poly(HEMA-MAPA) were 0.12 +/- 0.01 and 1.79 +/- 0.76 according to ACD/logP algorithm program, respectively. Stability of the radiolabeled compound was investigated in time intervals given as 0, 30, 60, 180, and 1440min. It was found that I-131-mag-poly(HEMA-MAPA) existed as a stable complex in rat serum within 60min. After that, biodistribution and scintigraphy studies were carried out by using albino Wistar rats. It was determined that the most important I-131 activity uptake was observed in the breast, the ovary, and the pancreas. Scintigraphy studies well supported biodistribution results. Copyright (c) 2013 John Wiley & Sons, Ltd.
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    In vivo biodistribution of 131I labeled bleomycin (BLM) and isomers (A2 and B2) on experimental animal models
    Avcibasi, U; Demiroglu, H; Ünak, P; Müftüler, FZB; Içhedef, ÇA; Gümüser, FG
    Bleomycins (BLMs; BLM, A2, and B2) were labeled with I-131 and radiopharmaceutical potentials were investigated using animal models in this study. Quality control procedures were carried out using thin layer radiochromatography (TLRC), high performance liquid chromatography (HPLC), and liquid chromatography (LC/MS/MS). Labeling yields of radiolabeled BLMs were found to be 90, 68, and 71%, respectively. HPLC chromatograms were taken for BLM and cold iodinated BLM (I-127-BLM). Five peaks were detected for BLM and three peaks for I-127-BLM in the HPLC studies. Two peaks belong to isomers of BLM. The isomers of BLM were purified with using HPLC. Biological activity of BLM was determined on male Albino Wistar rats by biodistribution and scintigraphic studies were performed for BLMs by using New Zelland rabbits. The biodistribution results of I-131-BLM showed high uptake in the stomach, the bladder, the prostate, the testicle, and the spinal cord in rats. Scintigraphic results on rabbits agrees with that of biodistributional studies on rats. The scintigraphy of radiolabeled isomers (I-131-A2 and I-131-B2) are similiarly found with that of I-131-BLM.
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    Investigation of therapeutic efficiency of phenytoin (PHT) labeled with radioactive 131I in the cancer cell lines
    Uzaras, C; Avcibasi, U; Demiroglu, H; Medine, EI; Kilçar, AY; Müftüler, FZB; Ünak, P
    The aim of this study is to determine the incorporations of PHT radiolabeled with I-131 (I-131-PHT) on U-87 MG, Daoy and A549 cancerous cell lines. For this, cold and radio-labeling studies were carried out. The radio-labeling yield of I-131-PHT was obtained about 95 %. Subsequently, cell culture studies were carried out and radio-labeling yields of I-131, I-131-PHT on U-87 MG, Daoy and A549 cancerous cells were investigated. Cell culture studies demonstrated that the incorporation values of (IPHT)-I-131 on the three cell lines decreased with increasing radioactivity. Consequently, I-131-PHT may be a good radiopharmaceutical for targeting radionuclide therapy of Central Nervous System Tumors.
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    Radiolabeling of Bleomycin-Glucuronide with 131I and Biodistribution Studies Using Xenograft Model of Human Colon Tumor in Balb/C Mice
    Demiroglu, H; Avcibasi, U; Ünak, P; Müftüler, FZB; Içhedef, ÇA; Gümüser, FG; Sakarya, S
    Bleomycin-glucuronide (BLMG) is the glucuronide conjugate of BLM. In the present study, BLMG was primarily enzymatically synthesized by using a microsome preparate separated from rat liver, labeled with I-131 by iodogen method with the aim of generating a radionuclide-labeled prodrug, and investigated its bioaffinities with tumor-bearing Balb/C mice. Quality control procedures were carried out using thin-layer radiochromatography and high-performance liquid chromatography. Tumor growing was carried out by following Caco-2 cell inoculation into mice. Radiolabeling yield was found to be about 65%. Results indicated that I-131-labeled BLMG (I-131-BLMG) was highly stable for 24 hours in human serum. Biodistribution studies were carried out with male Albino Wistar rats and colorectal adenocarcinoma tumor-bearing female Balb/C mice. The biodistribution results in rats showed high uptake in the prostate, the large intestine, and the spinal cord. In addition to this, scintigraphic results agreed with those of biodistributional studies. Xenography studies with tumor-bearing mice demonstrated that tumor uptakes of I-131-BLM and I-131-BLMG were high in the first 30 minutes postinjection. Tumor-bearing animal studies demonstrated that I-131-BLMG was specially retained in colorectal adenocarcinoma with high tumor uptake. Therefore, I-131-BLMG can be proven to be a promising imaging and therapeutic agent, especially for colon cancer in nuclear medical applications.
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    Synthesis and biodistribution of novel magnetic-poly(HEMA-APH) nanopolymer radiolabeled with iodine-131 and investigation its fate in vivo for cancer therapy
    Avcibasi, U; Avcibasi, N; Akalin, HA; Ediz, M; Demiroglu, H; Gümüser, FG; Özçaliskan, E; Türkcan, C; Uygun, DA; Akgöl, S
    Herein, we investigated the biological uptake, distribution, and radiopharmaceutical potential of a novel molecule based on 2-hydroxyethyl methacrylate (HEMA) and anilinephtalein (APH) in the metabolism of Albino Wistar rats. In order to achieve this, we synthesized APH using organic synthesis methods and copolymerized APH with HEMA using a common polymerization method, surfactant-free emulsion polymerization. In the presence of Fe3O4 particles, we obtained a new generation magnetic-nano-scale polymer, magnetic-poly(HEMA-APH). This new molecule was chemically identified and approved by several characterization methods using Fourier transform infrared spectroscopy, scanning electron microscope, energy dispersive X-ray spectroscopy, electron spin resonance, atomic force microscope, and Zeta particle-size analysis. To evaluate the biological activity in live metabolism and anti-cancer potential of mag-poly(HEMA-APH), molecule was radioiodinated by a widely used labeling technique, iodogen method, with a gamma diffuser radionuclide, I-131. Thin-layer radiochromatography experiments demonstrated that I-131 binded to nanopolymer with the labeling yield of 90 %. Lipophilicity and stability experiments were conducted to determine the condition of cold and labeled mag-poly(HEMA-APH) in rat blood and lipid medium. Results demonstrated that radioiodinated molecule stayed as an intact complex in rat metabolism for 24 h and experimental lipophilicity was determined as 0.12 +/- A 0.02. In vivo results obtained by imaging and biological distribution experiments indicated that mag-poly(HEMA-APH) labeled with I-131 [I-131-mag-poly(HEMA-APH)] highly incorporated into tissues of the uterus, the ovarian, the prostate, and the lungs in rat metabolism. Based on these results, it may be evaluated that novel mag-poly(HEMA-APH) molecule labeled with I-131 is a compound which has a significant potential for being used as an anti-cancer agent. Certain results can only be obtained whether this molecule is applied to adenocarcinoma cell models and tumor-bearing animals.
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    Investigation of Therapeutic Efficiency of Bleomycin and Bleomycin-Glucuronide Labeled with 131I on the Cancer Cell Lines
    Ediz, M; Avcibasi, U; Ünak, P; Müftüler, FZB; Medine, EI; Kilçar, AY; Demiroglu, H; Gümüser, FG; Sakarya, S
    The aim of this study is to determine the incorporations of radiolabeled bleomycin (I-131-BLM) and bleomycin-glucuronide (I-131-BLMGLU) on PC-3 (human prostate carcinoma cell line), Caco-2 (human colon adenocarcinoma cell line), Hutu-80 (Human Duodenum adenocarcinoma cell line), and A549 (Human lung adenocarcinoma epithelial cell line) cancerous cell lines. For this purpose, BLM and BLMGLU enyzmatically synthesized were labeled with I-131, quality control studies were done and the incorporation yields of I-131-BLM and I-131-BLMGLU on these cell lines were measured. Quality-control studies showed that the radiolabeling yields were obtained as 95% and 90% for I-131-BLM and I-131-BLMGLU, respectively. Also, as a result of the cell culture studies, it was found that I-131-BLM and I-131-BLMGLU had higher incorporation on PC-3 cells than that of other cell lines. In addition to this, it was reported that the incorporation yield of I-131-BLMGLU was higher than that I-131-BLM. At the end of the study, cytotoxicities of BLM and BLMGLU on PC-3 cancerous cell line were inspected and fluorescent images of BLM and BLMGLU were taken on PC-3 cells by using fluorescein isothiocyanate. In conclusion, cell culture studies demonstrated that the incorporation values of I-131-BLMGLU on the four cell lines were about five to six times higher than I-131-BLM. Radiolabeled glucuronide derivatives can be used in cancer therapy and tumor imaging, depending on the properties of radioiodine for the beta-glucuronidase-rich tissues because glucuronidation leads to rapid and higher incorporation on adenocarcinoma cells.
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    The effect of radiolabeled antibiotics on biofilm and microorganism within biofilm
    Avcibasi, U; Demiroglu, H; Sakarya, S; Ünak, P; Tekin, V; Ates, B
    The aim of this study was to investigate the I-131 and I-127 labeled linezolid and moxifloxacin effects of minimum inhibitory concentration, and minimum bactericidal concentration on mature biofilm and microorganism within the biofilm. Linezolid and moxifloxacin were labeled with I-131 and I-127 and chromatography studies were carried out with thin layer radiochromatograpy and high-pressure liquid radiochromatography techniques. Specific activities of radiolabeled LZD and MXF was found to be 53.3 +/- 3.1 and 127.3 +/- 1.1 MBq/A mu mol for [I-131]LZD and 7.6 +/- 0.02 and 55.6 +/- 0.8 MBq/A mu mol for [I-131]MXF, respectively. The minimum inhibitory concentration and Time-Kill of Linezolid and moxifloxacin alone and their I-131 and I-127 labeled forms were tested with a standard strain of meticillin-susceptible StaphylocA +/- ccus aureus. MIC values of LNZ and MXF were 2.96 nmol/mL (1 A mu g/ml) and 0.141 nmol/mL (0.062 A mu g/ml). Time Kills of MXF and LZD were found to be 0.06 and 1 mu g, respectively. Antibiotics labeled with beta-emitting radioactive molecule may be a new theranostics strategy for biofilm infections.
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    Investigation of Radiopharmaceutical Potential of Magnetic Poly(HEMA-APH) Nanoparticles Radiolabeled with Iodine-131 on Experimental Animals
    Avcibasi, U; Avcibasi, N; Gümüser, F; Uygun, D; Akgöl, S; Akalin, H; Ediz, M; Demiroglu, H; Özçaliskan, E; Türkcan, C